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Bindarit CCL2, CCL7 and CCL8 inhibitor

Catalog No.B2156
Size Price Stock Qty
10mM (in 1mL DMSO)
$154.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$119.00
In stock
25mg
$329.00
In stock
50mg
$469.00
In stock
200mg
$1,169.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Bindarit

Protocol

Cell experiment [1]:

Cell lines

Rat vascular smooth muscle cells (VSMCs)

Preparation method

The solubility of this compound in DMSO is > 16.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

10 ~ 300 μM

Applications

At the doses of 100 and 300 μM, Bindarit significantly inhibited PDGF-BB-induced rat VSMC proliferation by 27% and 42%, respectively. Moreover, in VSMCs stimulated with PDGF-BB, Bindarit (10 ~ 300 μM) inhibited MCP-1 production in a concentration-dependent manner.

Animal experiment [1]:

Animal models

ApoE-/- mice

Dosage form

100 mg/kg; p.o.; b.i.d.

Applications

In ApoE-/- mice, Bindarit significantly reduced the number of PCNA-positive cells as well as neointimal area. In neointimal lesion, Bindarit also reduced the relative content of F4/80-positive macrophages and the number of VSMCs by 66% and 30%, respectively.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Grassia G, Maddaluno M, Guglielmotti A, et al. The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemicmice[J]. Cardiovascular research, 2009, 84(3): 485-493.

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Chemical Properties

Cas No. 130641-38-2 SDF Download SDF
Chemical Name 2-[(1-benzylindazol-3-yl)methoxy]-2-methylpropanoic acid
Canonical SMILES CC(C)(C(=O)O)OCC1=NN(C2=CC=CC=C21)CC3=CC=CC=C3
Formula C19H20N2O3 M.Wt 324.37
Solubility >16.2mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Bindarit(AF-2838), an anti-inflammatory agent, is a selective inhibitor againstmonocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8[1].

MCP-1, MCP-2, and MCP-3 are inflammatory mediators that specifically stimulate the directional migration of T cells as well as monocytes and may play an important role in immune cell recruitment into sites of antigenic challenge [2].

In vitro: Bindarit inhibited MCP-1 and TNF-alpha production induced in monocytes by LPS and Candida albicans in a dose-dependent manner with the IC50 of 172 µM and 403 µM, respectively.The inhibition of LP-induced MCP-1 production by Bindarit has been associated with the reduced levels of MCP-1 mRNA transcripts with the IC50 value of 75 µM. Bindaritexihibited an inhibitory effect in the production of MCP-1 by LPS-stimulated MM6 cells with an IC50 of 425 μM, without affecting the release of IL-8 or IL-6[3].Administration of bindarit (10-300 μM) reduced rat vascular smooth muscle cell (VSMC) proliferation, migration, and invasion[4].

In vivo: In NZB/W mice model with lupus nephritis, oral treatment of bindarit prolonged survival and delayed the onset of proteinuria [3]. In rats treated with bindarit (200 mg/kg/day), bindarit resulted in a 39% reduction of balloon injury-induced neointima formation at day 14 without affecting re-endothelialization. Bindarit reduced the number of medial and neointimal proliferating cells at day 7 by 54 and 30%, respectively. In hypercholesterolaemicapoE(-/-) mice, administration of bindarit reduced the number of proliferating cells by 42%at day 7 after carotid injury and inhibited of neointima formation by 47% at day 28. In neointimal lesions of apoE(-/-) mice treated with bindarit, data analysis of the cellular composition showed that the relative content of macrophages and the number of VSMCs were reduced by 66 and 30%, respectively, compared with the control group[4].

References:
[1]. Zoja C, Corna D, Benedetti G, et al. Bindarit retards renal disease and prolongs survival in murine lupus autoimmune disease[J]. Kidney international, 1998, 53(3): 726-734.
[2]. Taub D D, Proost P, Murphy W J, et al. Monocyte chemotactic protein-1 (MCP-1),-2, and-3 are chemotactic for human T lymphocytes[J]. Journal of Clinical Investigation, 1995, 95(3): 1370.
[3]. Sironi M, Guglielmotti A, Polentarutti N, et al. A small synthetic molecule capable of preferentially inhibiting the production of the CC chemokine monocyte chemotactic protein-1[J]. European cytokine network, 1999, 10(3): 437-442.
[4]. Grassia G, Maddaluno M, Guglielmotti A, et al. The anti-inflammatory agent bindarit inhibits neointima formation in both rats and hyperlipidaemicmice[J]. Cardiovascular research, 2009, 84(3): 485-493.